title: Pharmacokinetics, tissue distribution and relative bioavailability of puerarin solid lipid nanoparticles following oral administration.
abstract: Puerarin has various pharmacological effects; however, poor water-solubility and low oral bioavailability limit its clinical utility. A delivery system of solid lipid nanoparticles could enhance its oral absorption. The objective of this study was to investigate the pharmacokinetics, tissue distribution and relative bioavailability of puerarin in rats after a single dose intragastric administration of puerarin solid lipid nanoparticles (Pue-SLNs). The puerarin concentrations in plasma and tissues were determined by rapid resolution liquid chromatography electrospray ionization-tandem mass spectrometry. The C(max) value of puerarin after the administration of Pue-SLNs was significantly higher than that obtained with puerarin suspension (0.33±0.05 μg/mL vs. 0.16±0.06 μg/mL, P<0.01). The T(max) value after the administration of the Pue-SLNs was significantly shorter than that after puerarin suspension administration (40±0 min vs. 110±15.49 min, P<0.01). The AUC(0→t) values of puerarin were 0.80±0.23 mg h/L, and 2.48±0.30 mg h/L after administration of the puerarin suspension and Pue-SLNs, respectively. Following administration of the Pue-SLNs, tissue concentrations of puerarin also increased, especially in the target organs such as the heart and brain. These data suggest that SLNs are a promising delivery system to enhance the oral bioavailability of puerarin.
authors.affiliation: The Second Affiliated Hospital of Guangzhou Medical University, Guangzhou Institute of Cardiovascular Disease, Guangzhou 510260, China.
authors.forename: Cheng-Feng
authors.initials: CF
authors.lastname: Luo
authors.forename: Mu
authors.initials: M
authors.lastname: Yuan
authors.forename: Min-Sheng
authors.initials: MS
authors.lastname: Chen
authors.forename: Shi-Ming
authors.initials: SM
authors.lastname: Liu
authors.forename: Liu
authors.initials: L
authors.lastname: Zhu
authors.forename: Bi-Yun
authors.initials: BY
authors.lastname: Huang
authors.forename: Xia-Wen
authors.initials: XW
authors.lastname: Liu
authors.forename: Wen
authors.initials: W
authors.lastname: Xiong
mesh_terms: D000284:Administration, Oral; D000818:Animals; D019540:Area Under Curve; D001682:Biological Availability; D002853:Chromatography, Liquid / Q000379:methods; D005260:Female; D007529:Isoflavones / Q000008:administration & dosage / Q000493:pharmacokinetics*; D008055:Lipids / Q000737:chemistry; D008297:Male; D053758:Nanoparticles; D051381:Rats; D017207:Rats, Sprague-Dawley; D021241:Spectrometry, Mass, Electrospray Ionization / Q000379:methods; D053719:Tandem Mass Spectrometry / Q000379:methods; D014018:Tissue Distribution; D014665:Vasodilator Agents / Q000008:administration & dosage / Q000493:pharmacokinetics*
chemical_list: D007529:Isoflavones; D008055:Lipids; D014665:Vasodilator Agents; C033607:puerarin